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Development of Potent G Protein Pathway-Biased GPR183 Agonists

Kaustubh R. Bhuskute Asmita Manandhar V. M. S. Kjær Francesco Casartelli G. Hjortø Maria Ioanna Koutsaki Udhayabhaskar Sathyanarayanan Emilia Hjortkilde Rita Turcio M. Rosenkilde T. Ulven Elisabeth Rexen Ulven

Jul 2026 · bioRxiv · 0 citations

Biology

TL;DR

The detailed structure-activity investigations and optimizations led to the identification of full agonists for GPR183 with complete bias for Gαi protein signaling and low nanomolar potency, including 63 (TUG-2604) with potency and efficacy similar to 7α,25-OHC.

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